JP6311315B2 - Mucosal ointment - Google Patents
Mucosal ointment Download PDFInfo
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- JP6311315B2 JP6311315B2 JP2014000780A JP2014000780A JP6311315B2 JP 6311315 B2 JP6311315 B2 JP 6311315B2 JP 2014000780 A JP2014000780 A JP 2014000780A JP 2014000780 A JP2014000780 A JP 2014000780A JP 6311315 B2 JP6311315 B2 JP 6311315B2
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- 239000002674 ointment Substances 0.000 title claims description 53
- 229930195733 hydrocarbon Natural products 0.000 claims description 19
- 150000002430 hydrocarbons Chemical class 0.000 claims description 19
- 239000004215 Carbon black (E152) Substances 0.000 claims description 17
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 17
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 17
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 17
- 239000000811 xylitol Substances 0.000 claims description 17
- 235000010447 xylitol Nutrition 0.000 claims description 17
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 17
- 229960002675 xylitol Drugs 0.000 claims description 17
- 150000005846 sugar alcohols Chemical class 0.000 claims description 15
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 claims description 10
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 claims description 10
- 229920002807 Thiomer Polymers 0.000 claims description 6
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 5
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims description 5
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims description 5
- 229960002920 sorbitol Drugs 0.000 claims description 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 3
- 239000004386 Erythritol Substances 0.000 claims description 3
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 claims description 3
- 229930195725 Mannitol Natural products 0.000 claims description 3
- 235000019414 erythritol Nutrition 0.000 claims description 3
- 229940009714 erythritol Drugs 0.000 claims description 3
- 239000000594 mannitol Substances 0.000 claims description 3
- 235000010355 mannitol Nutrition 0.000 claims description 3
- 229960001855 mannitol Drugs 0.000 claims description 3
- 239000000600 sorbitol Substances 0.000 claims description 3
- 235000010356 sorbitol Nutrition 0.000 claims description 3
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 claims 1
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 claims 1
- 229940099259 vaseline Drugs 0.000 claims 1
- 238000004898 kneading Methods 0.000 description 20
- 239000001768 carboxy methyl cellulose Substances 0.000 description 16
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 16
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 16
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 13
- 210000004400 mucous membrane Anatomy 0.000 description 10
- 230000000052 comparative effect Effects 0.000 description 6
- 235000019271 petrolatum Nutrition 0.000 description 6
- MPDGHEJMBKOTSU-YKLVYJNSSA-N 18beta-glycyrrhetic acid Chemical compound C([C@H]1C2=CC(=O)[C@H]34)[C@@](C)(C(O)=O)CC[C@]1(C)CC[C@@]2(C)[C@]4(C)CC[C@@H]1[C@]3(C)CC[C@H](O)C1(C)C MPDGHEJMBKOTSU-YKLVYJNSSA-N 0.000 description 4
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 210000000214 mouth Anatomy 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 229960001927 cetylpyridinium chloride Drugs 0.000 description 3
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 description 3
- 210000002200 mouth mucosa Anatomy 0.000 description 3
- 239000002994 raw material Substances 0.000 description 3
- 210000000664 rectum Anatomy 0.000 description 3
- 239000003871 white petrolatum Substances 0.000 description 3
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 2
- MPDGHEJMBKOTSU-UHFFFAOYSA-N Glycyrrhetinsaeure Natural products C12C(=O)C=C3C4CC(C)(C(O)=O)CCC4(C)CCC3(C)C1(C)CCC1C2(C)CCC(O)C1(C)C MPDGHEJMBKOTSU-UHFFFAOYSA-N 0.000 description 2
- 239000004264 Petrolatum Substances 0.000 description 2
- 229910000831 Steel Inorganic materials 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 229960000458 allantoin Drugs 0.000 description 2
- FUWUEFKEXZQKKA-UHFFFAOYSA-N beta-thujaplicin Chemical compound CC(C)C=1C=CC=C(O)C(=O)C=1 FUWUEFKEXZQKKA-UHFFFAOYSA-N 0.000 description 2
- 238000013329 compounding Methods 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 229960003720 enoxolone Drugs 0.000 description 2
- 238000009499 grossing Methods 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 210000003928 nasal cavity Anatomy 0.000 description 2
- 229940066842 petrolatum Drugs 0.000 description 2
- GEYJUFBPCGDENK-UHFFFAOYSA-M sodium;3,8-dimethyl-5-propan-2-ylazulene-1-sulfonate Chemical compound [Na+].CC(C)C1=CC=C(C)C2=C(S([O-])(=O)=O)C=C(C)C2=C1 GEYJUFBPCGDENK-UHFFFAOYSA-M 0.000 description 2
- 239000010959 steel Substances 0.000 description 2
- 210000001215 vagina Anatomy 0.000 description 2
- WJLVQTJZDCGNJN-UHFFFAOYSA-N Chlorhexidine hydrochloride Chemical compound Cl.Cl.C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 WJLVQTJZDCGNJN-UHFFFAOYSA-N 0.000 description 1
- SNPLKNRPJHDVJA-ZETCQYMHSA-N D-panthenol Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCCO SNPLKNRPJHDVJA-ZETCQYMHSA-N 0.000 description 1
- BIVBRWYINDPWKA-VLQRKCJKSA-L Glycyrrhizinate dipotassium Chemical compound [K+].[K+].O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C([O-])=O)[C@@H]1O[C@H](C([O-])=O)[C@@H](O)[C@H](O)[C@H]1O BIVBRWYINDPWKA-VLQRKCJKSA-L 0.000 description 1
- 239000002998 adhesive polymer Substances 0.000 description 1
- TUFYVOCKVJOUIR-UHFFFAOYSA-N alpha-Thujaplicin Natural products CC(C)C=1C=CC=CC(=O)C=1O TUFYVOCKVJOUIR-UHFFFAOYSA-N 0.000 description 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 1
- 229960004504 chlorhexidine hydrochloride Drugs 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 229960003957 dexamethasone Drugs 0.000 description 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 1
- 229940101029 dipotassium glycyrrhizinate Drugs 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 235000003599 food sweetener Nutrition 0.000 description 1
- 239000003205 fragrance Substances 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 230000007721 medicinal effect Effects 0.000 description 1
- 210000004877 mucosa Anatomy 0.000 description 1
- 229940101267 panthenol Drugs 0.000 description 1
- 235000020957 pantothenol Nutrition 0.000 description 1
- 239000011619 pantothenol Substances 0.000 description 1
- -1 polyethylene terephthalate Polymers 0.000 description 1
- 229920000139 polyethylene terephthalate Polymers 0.000 description 1
- 239000005020 polyethylene terephthalate Substances 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 238000005096 rolling process Methods 0.000 description 1
- 210000003296 saliva Anatomy 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 229960002117 triamcinolone acetonide Drugs 0.000 description 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 description 1
- 229930007845 β-thujaplicin Natural products 0.000 description 1
Description
本発明は、口腔、鼻腔、直腸、膣等の粘膜に適用する軟膏に関する。 The present invention relates to an ointment to be applied to mucous membranes such as oral cavity, nasal cavity, rectum and vagina.
従来から、粘膜適用型の付着製剤として、各種剤型が試みられている。例えば、口腔粘膜に付着させ、全身性の持続性または徐放性を目的とする錠剤が試みられている（特許文献１）。しかし、錠剤は異物感があり使用感が良くないという欠点がある。変形自在な製剤としてゲル剤、軟膏があり、今までにいくつか報告がなされているが（特許文献２〜４）、これらは製剤中に水分を含むため、強力な付着性を期待できるものではない。
水分を含まない軟膏についても試みられているが（特許文献５）、このような水分を含まない軟膏中に配合される油性基剤は特有の粘性を有しているため、粘膜に付きやすい性質がある。よって、これに付着性高分子を配合すれば、粘膜への付きやすさはさらに増す。しかし、目的部位以外の粘膜面にも付着しやすいという点で利便性（使用感）が損なわれていた。例えば口腔粘膜に軟膏を塗布して口を閉じると、患部以外の歯面などにも製剤が付着して、使用性が悪いばかりでなく、塗布量の損失により効果を期待できない場合がありうるし、また、有効成分を含有している場合は、薬効を十分に発揮できない場合があった。
Conventionally, various dosage forms have been tried as adhesion preparations for mucosal application. For example, a tablet that is attached to the oral mucosa and is aimed at systemic sustainability or sustained release has been attempted (Patent Document 1). However, tablets have a drawback that they have a foreign body feeling and are not good to use. There are gels and ointments as deformable preparations, and some reports have been made so far (Patent Documents 2 to 4). However, since these contain water in the preparations, strong adhesiveness cannot be expected. Absent.
Although an attempt has been made to use an ointment that does not contain water (Patent Document 5), since the oily base compounded in such an ointment that does not contain water has a specific viscosity, it tends to adhere to the mucous membrane. There is. Therefore, if an adhesive polymer is blended with this, the ease of attachment to the mucous membrane is further increased. However, convenience (feeling of use) has been impaired in that it easily adheres to mucosal surfaces other than the target site. For example, if you apply an ointment to the oral mucosa and close the mouth, the preparation will adhere to the tooth surface other than the affected area, not only the usability is bad, but the effect may not be expected due to the loss of the application amount, Moreover, when an active ingredient was contained, there existed a case where a medicinal effect could not fully be exhibited.
本発明は、適用する粘膜への付着性に優れ、かつ、適用箇所以外の粘膜には付着しにくい、利便性（使用感）の高い粘膜適用軟膏を提供することを課題とする。 An object of the present invention is to provide a mucous membrane ointment that is excellent in adhesion to the applied mucous membrane and is difficult to adhere to mucous membranes other than the application site and has high convenience (use feeling).
本発明者らは鋭意検討を行った結果、粘膜付着性高分子としてカルボキシメチルセルロースナトリウム及びポリアクリル酸ナトリウムから選択される少なくとも１種を使用する場合は、糖アルコールを特定量配合した場合に限って軟膏表面が水分で濡れるとき表面が滑らかになる性質を見出した。
かかる知見に基づき完成した本発明の態様は、
（１）カルボキシメチルセルロースナトリウム及びポリアクリル酸ナトリウムから選択される少なくとも１種の粘膜付着性高分子、５〜５０質量％の糖アルコール及び油性基剤を含有することを特徴とする粘膜適用軟膏、
（２）糖アルコールがキシリトール、ソルビトール、マンニトール及びエリスリトールからなる群から選択される少なくとも１種である、（１）に記載の粘膜適用軟膏、
（３）油性基剤がゲル化炭化水素及び／またはワセリンである（１）に記載の粘膜適用軟膏、である。
As a result of intensive studies, the present inventors have found that when at least one selected from sodium carboxymethylcellulose and sodium polyacrylate is used as the mucoadhesive polymer, only when a specific amount of sugar alcohol is added. It was found that the surface of the ointment becomes smooth when wetted with water.
The aspect of the present invention completed based on such findings is as follows.
(1) A mucosa-applied ointment comprising at least one mucoadhesive polymer selected from sodium carboxymethylcellulose and sodium polyacrylate, 5 to 50% by mass of a sugar alcohol and an oily base,
(2) The mucosa-applied ointment according to (1), wherein the sugar alcohol is at least one selected from the group consisting of xylitol, sorbitol, mannitol, and erythritol,
(3) The mucosa-applied ointment according to (1), wherein the oily base is a gelled hydrocarbon and / or petrolatum.
本発明の粘膜適用軟膏は、粘膜に適用して十分な付着性を備えつつ、例えば口腔内に適用する場合は唾液による水分によって適用部分に塗布した軟膏の表面が滑らかになる。適用箇所以外への付着がしにくいので、利便性（使用感）の良い粘膜適用軟膏を提供することが可能となった。 The mucosa-applied ointment of the present invention is applied to the mucous membrane and has sufficient adhesiveness. For example, when applied to the oral cavity, the surface of the ointment applied to the application portion is smoothed by the moisture of saliva. Since it is difficult to adhere to places other than the application site, it has become possible to provide a mucosa-applied ointment with good convenience (use feeling).
本発明の粘膜適用軟膏は、粘膜付着性高分子カルボキシメチルセルロースナトリウム及びポリアクリル酸ナトリウムから選択される少なくとも１種、５〜５０質量％の糖アルコール及び油性基剤を含有する。 The mucosa-applied ointment of the present invention contains at least one selected from the mucoadhesive polymer sodium carboxymethylcellulose and sodium polyacrylate, 5 to 50% by mass of sugar alcohol and an oily base.
本発明のカルボキシメチルセルロースナトリウムまたはポリアクリル酸ナトリウムは、粘膜の水分で付着性を発揮するような高分子原料である。これら粘膜付着性高分子は単独でも２種類を組み合わせても用いることができる。本発明における粘膜付着性高分子の含量は、１質量％〜５０質量％が好ましい。 The sodium carboxymethylcellulose or sodium polyacrylate of the present invention is a polymer raw material that exhibits adhesiveness with mucous membrane moisture. These mucoadhesive polymers can be used alone or in combination of two kinds. The content of the mucoadhesive polymer in the present invention is preferably 1% by mass to 50% by mass.
本発明の糖アルコールとは、糖分子のカルボニル基が還元されて水酸基になることにより得られる鎖式多価アルコールを指す。本発明の糖アルコールは常温で固体の糖アルコールが好ましく、特にキシリトール、ソルビトール、マンニトール、エリスリトールが好ましい。これら糖アルコールは単独でも２種類以上を組み合わせても用いることができる。本発明の軟膏表面が滑らかになる効果の面、及び風味向上の観点から、キシリトールが最も好ましい。本発明における糖アルコールの含量は効果の点から、軟膏中に５質量％以上配合する必要がある。糖アルコールの好ましい含有量としては、粘膜適用軟膏中５〜５０質量％、更に好ましく５〜３０質量％である。 The sugar alcohol of the present invention refers to a chain polyhydric alcohol obtained by reducing a carbonyl group of a sugar molecule to a hydroxyl group. The sugar alcohol of the present invention is preferably a sugar alcohol that is solid at room temperature, and xylitol, sorbitol, mannitol, and erythritol are particularly preferable. These sugar alcohols can be used alone or in combination of two or more. Xylitol is most preferable from the viewpoint of smoothing the ointment surface of the present invention and from the viewpoint of improving the flavor. The content of the sugar alcohol in the present invention must be 5% by mass or more in the ointment from the viewpoint of the effect. The preferable content of the sugar alcohol is 5 to 50% by mass, more preferably 5 to 30% by mass in the mucous membrane ointment.
本発明の油性基剤には、通常の油性軟膏に用いる原料から選択することができるが、白色ワセリン、黄色ワセリン等のワセリン類、ゲル化炭化水素が好ましい。本発明における油性基剤の含量は３５〜９０質量％が好ましい。 The oily base of the present invention can be selected from the raw materials used in ordinary oily ointments, but petrolatums such as white petrolatum and yellow petrolatum, and gelled hydrocarbons are preferred. The content of the oily base in the present invention is preferably 35 to 90% by mass.
本発明の粘膜適用軟膏は、実質的に水を含まない。本発明でいう実質的に水を含まないとは、本発明の効果に影響を及ぼさない程度の少量の水（例えば原料中に含まれる微量の水分）を含むことは許容範囲にあるという意味である。具体的には、軟膏中、水分量は５質量％以下、好ましくは３質量％以下である。本発明の粘膜適用軟膏中に水を含むと、粘膜適用時に軟膏表面が滑らかになる効果が期待できなくなるからである。 The mucosa-applied ointment of the present invention is substantially free of water. The term “substantially free of water” as used in the present invention means that it is acceptable to include a small amount of water that does not affect the effect of the present invention (for example, a small amount of water contained in the raw material). is there. Specifically, the amount of water in the ointment is 5% by mass or less, preferably 3% by mass or less. This is because if the mucosa-applied ointment of the present invention contains water, the effect of smoothing the ointment surface upon application of the mucosa cannot be expected.
本発明の粘膜適用軟膏は、例えば口腔内、鼻腔、直腸、膣等に適用することができる。また、治療目的の軟膏としたいならば、適切な有効成分を配合することができる。優れた使用感とするために、甘味剤、香料を適宜配合することができる。
本発明の粘膜適用軟膏の製造方法は、それぞれの成分を適切な製造機で均一なペースト状の軟膏となるように混合して製造する。
The mucosa-applied ointment of the present invention can be applied to the oral cavity, nasal cavity, rectum, vagina and the like. Moreover, if it is desired to make an ointment for therapeutic purposes, an appropriate active ingredient can be blended. In order to obtain an excellent feeling of use, a sweetener and a fragrance can be appropriately blended.
In the method for producing a mucous membrane-applied ointment of the present invention, the respective components are mixed and produced by an appropriate production machine so as to form a uniform paste-like ointment.
以下に、実施例、比較例および試験例を示し、本発明を詳細に説明する。 Hereinafter, the present invention will be described in detail with reference to Examples, Comparative Examples and Test Examples.
（実施例１）
ゲル化炭化水素65質量％、キシリトール5質量％、ポリアクリル酸ナトリウム30質量％を均一になるように混和練合して軟膏を製造した。
Example 1
An ointment was produced by mixing and kneading 65% by mass of gelled hydrocarbon, 5% by mass of xylitol and 30% by mass of sodium polyacrylate so as to be uniform.
（実施例２）
ゲル化炭化水素50質量％、キシリトール20質量％、ポリアクリル酸ナトリウム30質量％を均一になるように混和練合して軟膏を製造した。
(Example 2)
An ointment was produced by mixing and kneading 50% by mass of gelled hydrocarbon, 20% by mass of xylitol, and 30% by mass of sodium polyacrylate so as to be uniform.
（実施例３）
ゲル化炭化水素65質量％、Ｄ−ソルビトール5質量％、ポリアクリル酸ナトリウム30質量％を均一になるように混和練合して軟膏を製造した。
（実施例４）
ゲル化炭化水素75質量％、キシリトール5質量％、カルボキシメチルセルロースナトリウム20質量％を均一になるように混和練合して軟膏を製造した。
(Example 3)
An ointment was produced by mixing and kneading 65% by mass of gelled hydrocarbon, 5% by mass of D-sorbitol, and 30% by mass of sodium polyacrylate so as to be uniform.
Example 4
An ointment was produced by mixing and kneading 75% by mass of gelled hydrocarbon, 5% by mass of xylitol, and 20% by mass of sodium carboxymethylcellulose so as to be uniform.
（実施例５）
ゲル化炭化水素60質量％、キシリトール20質量％、カルボキシメチルセルロースナトリウム20質量％を均一になるように混和練合して軟膏を製造した。
(Example 5)
An ointment was produced by mixing and kneading 60% by mass of gelled hydrocarbon, 20% by mass of xylitol and 20% by mass of sodium carboxymethyl cellulose so as to be uniform.
（実施例６）
ゲル化炭化水素75質量％、Ｄ−ソルビトール5質量％、カルボキシメチルセルロースナトリウム20質量％を均一になるように混和練合して軟膏を製造した。
（実施例７）
ゲル化炭化水素59.9質量％、キシリトール30質量％、カルボキシメチルセルロースナトリウム10質量％、トリアムシノロンアセトニド0.1質量％を均一になるように混和練合して軟膏を製造した。
(Example 6)
An ointment was produced by mixing and kneading 75% by mass of gelled hydrocarbon, 5% by mass of D-sorbitol, and 20% by mass of sodium carboxymethyl cellulose so as to be uniform.
(Example 7)
An ointment was produced by uniformly kneading and kneading 59.9% by mass of gelled hydrocarbon, 30% by mass of xylitol, 10% by mass of sodium carboxymethylcellulose, and 0.1% by mass of triamcinolone acetonide.
（実施例８）
ゲル化炭化水素59.98質量％、キシリトール30質量％、カルボキシメチルセルロースナトリウム10質量％、アズレンスルホン酸ナトリウム0.02質量％を均一になるように混和練合して軟膏を製造した。
(Example 8)
An ointment was produced by uniformly kneading and kneading 59.98% by mass of gelled hydrocarbon, 30% by mass of xylitol, 10% by mass of sodium carboxymethylcellulose, and 0.02% by mass of sodium azulenesulfonate.
（実施例９）
ゲル化炭化水素79.58質量％、キシリトール10質量％、カルボキシメチルセルロースナトリウム10質量％、アズレンスルホン酸ナトリウム0.02質量％、グリチルレチン酸0.3質量％、塩化セチルピリジニウム0.1質量％を均一になるように混和練合して軟膏を製造した。
Example 9
79.58% by mass of gelled hydrocarbon, 10% by mass of xylitol, 10% by mass of sodium carboxymethylcellulose, 0.02% by mass of sodium azulene sulfonate, 0.3% by mass of glycyrrhetinic acid, and 0.1% by mass of cetylpyridinium chloride were mixed and kneaded to be uniform. An ointment was produced.
（実施例１０）
ゲル化炭化水素39.3質量％、白色ワセリン40質量％、キシリトール10質量％、カルボキシメチルセルロースナトリウム10質量％、紫根エキス0.2質量％、グリチルレチン酸0.3質量％、クロルヘキシジン塩酸塩0.2質量％を均一になるように混和練合して軟膏を製造した。
(Example 10)
Uniform gelling hydrocarbons 39.3% by weight, white petrolatum 40% by weight, xylitol 10% by weight, sodium carboxymethylcellulose 10% by weight, purple root extract 0.2% by weight, glycyrrhetinic acid 0.3% by weight, chlorhexidine hydrochloride 0.2% by weight An ointment was produced by kneading.
（実施例１１）
ゲル化炭化水素59.4質量％、キシリトール30質量％、カルボキシメチルセルロースナトリウム10質量％、塩化セチルピリジニウム0.1質量％、アラントイン0.5質量％を均一になるように混和練合して軟膏を製造した。
(Example 11)
An ointment was produced by uniformly kneading and kneading 59.4% by mass of gelled hydrocarbon, 30% by mass of xylitol, 10% by mass of sodium carboxymethylcellulose, 0.1% by mass of cetylpyridinium chloride and 0.5% by mass of allantoin.
（実施例１２）
ゲル化炭化水素59.9質量％、キシリトール30質量％、カルボキシメチルセルロースナトリウム10質量％、デキサメタゾン0.1質量％を均一になるように混和練合して軟膏を製造した。
(Example 12)
An ointment was produced by uniformly kneading and kneading 59.9% by mass of gelled hydrocarbon, 30% by mass of xylitol, 10% by mass of sodium carboxymethylcellulose, and 0.1% by mass of dexamethasone.
（実施例１３）
白色ワセリン58.85質量％、キシリトール30質量％、カルボキシメチルセルロースナトリウム10質量％、グリチルリチン酸ジカリウム0.4質量％、塩化セチルピリジニウム0.05質量％、ヒノキチオール0.1質量％、アラントイン0.3質量％、パンテノール0.3質量％を均一になるように混和練合して軟膏を製造した。
(Example 13)
White petrolatum 58.85% by mass, xylitol 30% by mass, sodium carboxymethylcellulose 10% by mass, dipotassium glycyrrhizinate 0.4% by mass, cetylpyridinium chloride 0.05% by mass, hinokitiol 0.1% by mass, allantoin 0.3% by mass, panthenol 0.3% by mass An ointment was produced by mixing and kneading.
（比較例１）
ゲル化炭化水素70質量％、ポリアクリル酸ナトリウム30質量％を均一になるように混和練合して軟膏を製造した。
(Comparative Example 1)
An ointment was produced by mixing and kneading 70% by mass of gelled hydrocarbon and 30% by mass of sodium polyacrylate so as to be uniform.
（比較例２）
ゲル化炭化水素69質量％、キシリトール1質量％、ポリアクリル酸ナトリウム30質量％を均一になるように混和練合して軟膏を製造した。
(Comparative Example 2)
An ointment was produced by mixing and kneading 69% by mass of gelled hydrocarbon, 1% by mass of xylitol and 30% by mass of sodium polyacrylate so as to be uniform.
（比較例３）
ゲル化炭化水素80質量％、カルボキシメチルセルロースナトリウム20質量％を均一になるように混和練合して軟膏を製造した。
(Comparative Example 3)
An ointment was produced by mixing and kneading 80% by mass of gelled hydrocarbon and 20% by mass of sodium carboxymethyl cellulose so as to be uniform.
（比較例４）
ゲル化炭化水素79質量％、キシリトール1質量％、カルボキシメチルセルロースナトリウム20質量％を均一になるように混和練合して軟膏を製造した。
(Comparative Example 4)
An ointment was produced by mixing and kneading 79% by mass of gelled hydrocarbon, 1% by mass of xylitol and 20% by mass of sodium carboxymethyl cellulose so as to be uniform.
（試験例）
厚さ25μmのポリエチレンテレフタレートフィルム（縦25cm、横7cm、商品名：ルミラーフィルム、サンプラテック株式会社）に、実施例１〜６及び比較例１〜４の軟膏をそれぞれドクターナイフ（テスター産業株式会社）で縦20cm、横5cm、厚さ1.0mmに均一に伸ばして２０度に傾斜をつけた板（縦35cm、横14.5cm）に固定し、スチールボール（テスター産業株式会社 No.2 直径4.7625mm 重量0.45g）を軟膏の端から約10cm上方から転がし、軟膏の端からボールが止まるまでの転がった距離を測定した（試験１）。次に、軟膏表面を精製水で均一に濡らしてから15秒後に試験１と同じスチールボールを転がして、ボールが転がった距離を測定した（試験２）。その結果を表１〜３に示す。
(Test example)
A doctor knife (Tester Sangyo Co., Ltd.) was applied to each of the ointments of Examples 1 to 6 and Comparative Examples 1 to 4 on a polyethylene terephthalate film (25 cm long, 7 cm wide, trade name: Lumirror film, Samplertech Co., Ltd.) A steel ball (Tester Sangyo Co., Ltd. No.2 diameter 4.7625mm, weight 0.45) is fixed to a plate (length 35cm, width 14.5cm) that is uniformly extended to 20cm in length, 5cm in width and 1.0mm in thickness and inclined at 20 degrees. g) was rolled from about 10 cm above the end of the ointment, and the distance of rolling until the ball stopped from the end of the ointment was measured (Test 1). Next, after the surface of the ointment was uniformly wetted with purified water, the same steel ball as in Test 1 was rolled 15 seconds later, and the distance the ball was rolled was measured (Test 2). The results are shown in Tables 1-3.
油性基剤を配合した軟膏表面は粘着性があり、通常はボールが転がりにくい性質であるが、糖アルコールを配合し、水で濡らす時に表面の滑らかさが増してボールが転がるようになる。試験の結果、糖アルコールの配合量が５質量％以上では配合量を増すとボールが転がる距離が長くなっており、水に濡れた軟膏表面の滑らかさが増すことがわかった。 The ointment surface blended with an oily base is sticky and usually has a property that the ball does not roll easily, but when the sugar alcohol is blended and wetted with water, the surface becomes smooth and the ball rolls. As a result of the test, it was found that when the compounding amount of the sugar alcohol was 5% by mass or more, the distance that the ball rolls was increased when the compounding amount was increased, and the smoothness of the ointment surface wet with water was increased.
本発明の粘膜適用軟膏は、口腔粘膜や直腸等の粘膜に適用するのに適した軟膏状の医薬品、医薬部外品、化粧品、雑貨等を提供することが可能となった。 The mucosa-applied ointment of the present invention can provide ointment-like pharmaceuticals, quasi-drugs, cosmetics, miscellaneous goods, and the like suitable for application to mucous membranes such as oral mucosa and rectum.
Claims (2)
なくとも１種の粘膜付着性高分子、５〜５０質量％の糖アルコール、及びゲル化炭化水素及び／またはワセリンである油性基剤を含有し、前記油性基剤の含有量が３５〜９０質量％であることを特徴とする粘膜適用軟膏。 At least one mucoadhesive polymer selected from carboxymethylcellulose sodium and sodium polyacrylate, containing an oily base is 5 to 50 wt% sugar alcohols, and hydrocarbon gel and / or vaseline, wherein A mucosa-applied ointment , wherein the content of the oily base is 35 to 90% by mass .
群から選択される少なくとも１種である、請求項１に記載の粘膜適用軟膏。 The mucosa-applied ointment according to claim 1, wherein the sugar alcohol is at least one selected from the group consisting of xylitol, sorbitol, mannitol and erythritol.
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